• Title/Summary/Keyword: drug release

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Formulation and Pharmaceutical Properties of Local Mucoadhesive-Patch Preparation (국소치료용 구강점막패취의 제제설계 및 약제학적 특성)

  • Lee, Gye-Ju;Shu, Hyun-Joo;Lee, Duck-Geun;Park, Jong-Bum;Shin, Kwang-Hyun;Hwang, Sung-Joo
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.187-195
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    • 1998
  • In order to ameliorate disadvantages of buccal ointments and mucoadhesive tablets used for the treatment of aphthosis, a thin mucoadhesive patch containing triamcinolone acetoni de was designed and evaluated for the pharmaceutical properties. The adhesive gel layer consisting of Noveon AA-1, hydroxypropylcellulose-M and ethylcellulose N 100, and the protective gel layer of ethylcellulose N 100, Eudragit RSPO and castor oil have been formulated and various properties such as viscosity of drug gel layer, thickness, in vitro adhesion time, adhesive strength, surface pH, content uniformity and drug release are tested. The mean viscosity of drug-containing gel layer was found to increase with increasing amount of Noveon OAA-1 or hydroxypropylcellulose-M. The optimum formulation showed the thickness of 171 ${\mu}$m, surface pH of 4.6, in vitro adhesion time of 8 hours and adhesive strength of 272.7g/sheet. The drug content of each patch was relatively homogeneous with the value of 273${\pm}$6.77g. Drug release study showed that compared to mucoadhesive tablet, the patch showed a faster drug release. Drug release was delayed by hydroxypropylcellulose-M, but not by ethylcellulose N 100. The patches prepared were nonirritant and the muco adhesion was better than the commercial product (AftachR) on the market. Based on these results, this mucoadhesive patch is expected to be an effective dosage form for the treatment of aphthosis.

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Release Characteristics of Sulfadiazine Using Chitosan Matrices (키토산 매트릭스를 이용한 Sulfadiazine의 방출 특성)

  • 문일식;나재운
    • KSBB Journal
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    • v.11 no.6
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    • pp.676-680
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    • 1996
  • The characteristics of controlled drug release were studied for a biodegradable drug delivery system. A biodegradable chitosan matrix was prepared after swelling chitosan with 10%-acetic acid and adding sulfadiazine. The release behavior of sulfadiazine from the chitosan matrix was studied using the Higuchi's diffusion controlled model in phosphate buffer solutions of pH 7.4 and pH 1.2. The drug release time was delayed by increasing the content of sulfadiazine. The drug release at pH 7.4 was more delayed than that at pH 1.2. The reason is that chitosan has greater swelling abilities at low pH than at high pH. The apparent release rate constant(K) increased as the concentration of drug increased. In shoat, the formulation the biodegradable chitosan matrix to suppress the burst effect of drug release mechanism, which led to a sustained release pattern.

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Synthesis of Lactide/Hyaluronic Acid Polymer Membrane for the Application of Drug Delivery System (약물방출시스템 적용을 위한 락타이드/히아루론산 고분자 막의 제조)

  • Kim, Min-Su;Kwon, Ji-Young;Cheong, Seong-Ihl
    • Membrane Journal
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    • v.15 no.4
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    • pp.281-288
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    • 2005
  • The hyaluronic acid (HA) with excellent biocompatibility can be combined with lactide, the ester dimer of polylactide, with good biodegradability to produce biocompatible materials applicable to drug delivery system. By freeze drying method, HA and lactide were crosslinked with crosslinking agent, 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide. Degree of lactide and EDC reaction was determined by the analysis of nuclear magnetic resonance (NMR) spectroscopy. The degree of lactide and EDC reaction increased and swelling ratio decreased as the mole ratio of lactide to HA or crosslinking agent concentration increased or reaction temperature decreased. The drug release experiment result from membranes having different degree of lactide reaction showed that drug release rate reduced in proportion to the degree of lactide reaction. The drug release experiment result from drugs having different hyrodphobicity showed that the more hydrophobic drug was released more slowly.

Drug Release Behavior and Degradability of Microspheres Prepared using Water-Soluble Chitosan (수용성 키토산으로 제조한 미세구의 분해성과 약물 방출 거동)

  • 장미경;최창용;김원석;정영일;나재운
    • Polymer(Korea)
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    • v.28 no.4
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    • pp.291-297
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    • 2004
  • Water-soluble chitosan micro spheres were prepared by emulsification of chitosan solution in mineral oil followed by cross linking reaction with different amount of the cross linking agent (glutraraldehyde), different chitosan concentration. Then, the physicochemical properties such as morphological change by degradation, drug loading efficiency, and drug release profiles were investigated with the drug loaded water-soluble chitosan microspheres. Norfloxacin loaded water-soluble chitosan micro spheres showed excellent drug entrapping capacities without burst release caused by surface bound drug. The absence of the surface bound drug also confirmed by X-ray diffraction study. Degradation and drug release studies showed that the amount of the crosslinking agent played a crucial role for drug loading, release and degradation. The water-soluble chitosan micro spheres showed more sustained drug release profiles with slower degradation and larger particle size by increasing crosslinking agent.

Preparation and Characterization of Biodegradable Poly($\varepsilon$-caprolactone)/ Poly(ethylene oxide) Microcapsules Containing Erythromycin (에리트로마이신을 함유한 생분해성 폴리카프로락톤/폴리(에틸렌 옥사이드) 마이크로캡슐의 제조 및 특성)

  • 박수진;김승학;이재락;이해방;홍성권
    • Polymer(Korea)
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    • v.27 no.5
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    • pp.449-457
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    • 2003
  • The purposes of this work were the producing of a biodegradable poly($\varepsilon$-caprolactone) (PCL) / poly(ethylene oxide) (PEO) microcapsule and the analyzing of form and features for the manufacturing conditions which could be observed in a prospective drug delivery systems through drug release. The effects of emulsifier, emulsifier concentration, and stirring rate for the diameter and form of the microcapsules were observed using image analyzer and scanning electron microscope. The role of interfacial adhesion between PCL/PEO and drug was determined by contact angle measurements, and the drug release test of the microcapsules was characterized by UV/vis. spectra. As a result, the microcapsules were made in spherical fonns with a mean particle size of 170 nm∼68 $\mu$m. And the work of adhesion between water and PCL/PEO increased with increasing the content of PEO, probably due to the increased the hydrophilicity. It was also found that the drug release rate from the microcapsules significantly increased with increasing the content of PEO, which could be also attributed to the increasing of the hydrophilic groups or the degree of adhesion force at interfaces.

Controlled Release of Propranolol Hydrochloride and Indomethacin from Hollow Type Suppository Using Witepsol H-15 (Witepsol 중공좌제로부터의 염산프로프라놀롤 및 인도메타신의 방출제어)

  • Jin, Suk-Yeong;Gu, Yeong-Sun
    • YAKHAK HOEJI
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    • v.40 no.4
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    • pp.400-410
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    • 1996
  • In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

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New Coating Method for Sustained Drug Release: Surface Modification of ePTFE Grafts by inner coating PLGA

  • Kim, Hyeseon;Park, Seohyeon;Kim, Dae Joong;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.35 no.5
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    • pp.1333-1336
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    • 2014
  • Expanded polytetrafluoroethylene (ePTFE) grafts have been used as vascular access for many patients suffering from end stage renal disease. However, the vascular graft can cause significant clinical problems such as stenosis or thrombosis. For this reason, many studies have been performed to make drug eluting graft, but initial burst is major problem in almost drug eluting systems. Therefore we used biodegradable polymer to reduce initial burst and make sustained drug delivery. The ePTFE grafts were dipped into a paclitaxel-dissolved solution and then PLGA-dissolved solution was passed through the lumen of ePTFE. We analyzed whether the dose of paclitaxel is enough and the loading amount of PLGA on ePTFE graft increases according to the coating solution's concentration. Scanning electron microscope (SEM) images of various concentration of PLGA showed that the porous surface of graft was more packed with PLGA by tetrahydrofuran solution dissolved PLGA. In addition, in vitro release profiles of Ptx-PLGA graft demonstrated that early burst was gradually decreased as increasing the concentration of PLGA. These results suggest that PLGA coating of Ptx loaded graft can retard drug release, it is useful tool to control drug release of medical devices.

Synthesis and Drug Release Property of Poly(ethylene glycol-block-L-lactide-block-N-isopropylacrylamide) Triblock Copolymer (Poly(ethylene glycol-block-L-lactide-block-N-isopropylacrylamide) 삼중 블록 공중합체의 합성과 약물 방출성)

  • Jung, Sujin;Kim, Hong Sung
    • Textile Science and Engineering
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    • v.57 no.5
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    • pp.247-254
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    • 2020
  • Herein, novel linear block copolymers have been synthesized for use as a drug-eluting coating material in vascular grafts. Poly(ethylene glycol-block-L-lactide-block-N-isopropylacrylamide) triblock copolymers were prepared by stepwise polymerization from methoxy-terminated polyethylene glycol, i.e., anionic ring-opening polymerization of L-lactide followed by quasi-living polymerization of N-isopropylacrylamide. The chemical structures of the triblock copolymers were analyzed by FT-IR spectroscopy, 1H-NMR spectroscopy, and WAXD. The surface adhesion of triblock copolymers was evaluated for the substrate and model proteins. The drug release behavior of antiproliferative methotrexate was investigated according to the block ratio of the triblock copolymers. Viscosity increased significantly with increasing proportion of poly(N-isopropylacrylamide) block, whereas protein adhesion decreased with decreasing proportion of poly(L-lactide) block. Furthermore, methotrexate release increased with decreasing proportion of poly(L-lactide) block, and both the initial and sustained release increased with increasing proportion of poly(N-isopropyl acrylamide) block. This triblock copolymer can adjust the ratio of blocks to design effective drug release for specific applications.

Design and Optimization of Solid Dispersed Osmotic Pump Tablets of Aceclofenac, A Better Approach to Treat Arthritis

  • Edavalath, Sudeesh;Rao, B. Prakash
    • Journal of Pharmaceutical Investigation
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    • v.41 no.4
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    • pp.217-225
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    • 2011
  • The aim of this work was to prepare porous osmotic pump tablets for controlled delivery of Aceclofenac. Aceclofenac solid dispersion was prepared to improve the solubility by using the drug - carrier (Mannitol) ratio of 1:1. The osmotic pump tablets were prepared using the solid dispersed product of Aceclofenac. The formulation contains potassium chloride as osmotic agent, cellulose acetate as semipermeable membrane, poly ethylene glycol (PEG 4000) as pore former and sodium lauryl sulphate (SLS) as solubility enhancer. The formulations were designed by the general factors such as osmotic agent and pore former. All formulations were evaluated for various physical parameters and, the in vitro release studies were conducted as per USP. The drug release kinetic studies such as zero order, first order, and Higuchi and Korsmeyer peppas were determined and compared. All the formulations gave more controlled release compared to the marketed tablet studied. Numerical optimization techniques were applied to found out the best formulation by considering the parameter of in vitro drug release kinetics and dissolution profile standards. It was concluded that the porous osmotic pump tablets (F7) composed of Aceclofenac solid dispersion/Potassium chloride/Lactose/Sodium lauryl sulphate/Magnesium Stearate (400/40/95/10/5, mg/tab) and coating composition with Cellulose acetate/ PEG 4000 (60/40 %w/w) is the most satisfactory formulation. The porous osmotic pump tablets provide prolonged, controlled, and gastrointestinal environment-independent drug release.

Comparative Study of Spray Drying Method and Solvent Evaporation Method for Preparation of Biodegradable Microspheres Containing Nicotine and Triamcinolone Acetonide (니코틴과 트리암시놀론 아세토니드를 함유하는 생분해성 마이크로스피어의 제조시 분무건조법과 용매증발법의 비교)

  • Park, Sun-Young;Cho, Mi-Hyun;Lee, Jeong-Hwa;Kim, Dong-Woo;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.31 no.4
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    • pp.257-263
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    • 2001
  • The microspheres have been developed as a new drug delivery system. Although many particulate drug carriers, such as liposome, niosome and emulsion, have been introduced, injectable and biodegradable microspheres appears to be a particularly ideal delivery system because the local anesthesia is not necessary for the insertion of large implants and for the removal of the device after the drug release is finished. Biodegradable microspheres with nicotine and triamcinolone acetonide are prepared and evaluated. As biodegradible polymers, PLA (M.W. 15,000, PLA-0015), PLGA (M.W. 17,000, RG 502) and PLGA (M.W. 8,600, RG 502H) are used. This study attempted to prepare and evaluate the nicotine and triamcinolone acetonide-incorporated microspheres, which were prepared by two methods, solvent-evaporation and spray-drying methods. The microspheres, as a disperse system for injections, were evaluated by particle size, size distribution, entrapment efficiency, and in vitro drug release patterns. The differences of preparation method, partition coefficient, types of polymer, and preparation conditions of microspheres influence the particle size, entrapment efficiency, and in vitro drug release patterns.

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